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European Journal of Drug Metabolism and Pharmacokinetics

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https://www.readbyqxmd.com/read/27889876/population-pharmacokinetic-pharmacodynamic-modeling-of-5-fluorouracil-for-toxicities-in-rats
#1
Shinji Kobuchi, Yukako Ito, Toshiyuki Sakaeda
BACKGROUND AND OBJECTIVES: Myelosuppression is a dose-limiting toxicity of 5-fluorouracil (5-FU). Predicting the inter- and intra-patient variability in pharmacokinetics and toxicities of 5-FU may contribute to the individualized medicine. This study aimed to establish a population pharmacokinetic-pharmacodynamic model that could evaluate the inter- and intra-individual variability in the plasma 5-FU concentration, 5-FU-induced body weight loss and myelosuppression in rats. METHOD: Plasma 5-FU concentrations, body weight loss, and blood cell counts in rats following the intravenous administration of various doses of 5-FU for 4 days were used to develop the population pharmacokinetic-pharmacodynamic model...
November 26, 2016: European Journal of Drug Metabolism and Pharmacokinetics
https://www.readbyqxmd.com/read/27864798/pharmacokinetic-drug-interactions-with-panax-ginseng
#2
REVIEW
Meenakshi R Ramanathan, Scott R Penzak
Panax ginseng is widely used as an adaptogen throughout the world. The major active constituents of P. ginseng are ginsenosides. Most naturally occurring ginsenosides are deglycosylated by colonic bacteria to intestinal metabolites. Ginsenosides along with these metabolites are widely accepted as being responsible for the pharmacologic activity and drug interaction potential of ginseng. Numerous preclinical studies have assessed the influence of various ginseng components on cytochrome P450 (CYP), glucuronidation, and drug transport activity...
November 18, 2016: European Journal of Drug Metabolism and Pharmacokinetics
https://www.readbyqxmd.com/read/27858342/physiologically-based-pharmacokinetic-pbpk-modeling-of-pitavastatin-and-atorvastatin-to-predict-drug-drug-interactions-ddis
#3
Peng Duan, Ping Zhao, Lei Zhang
BACKGROUND: The disposition of statins varies and involves both metabolizing enzymes and transporters, making predictions of statin drug-drug interactions (DDIs) challenging. Physiologically based pharmacokinetic (PBPK) models have, however, demonstrated ability to predict complex DDIs. OBJECTIVE: In this study, PBPK models of two statins (pitavastatin and atorvastatin) were developed and applied to predict pitavastatin and atorvastatin associated DDIs. METHOD: Pitavastatin and atorvastatin PBPK models were developed using in vitro and human pharmacokinetic data in a population-based PBPK software (SimCYP(®)) by considering the contribution of both metabolizing enzymes and transporters to their overall pharmacokinetics...
November 17, 2016: European Journal of Drug Metabolism and Pharmacokinetics
https://www.readbyqxmd.com/read/27853934/evaluation-of-in-vitro-cytochrome-p450-inhibition-and-in-vitro-fate-of-structurally-diverse-n-oxide-metabolites-case-studies-with-clozapine-levofloxacin-roflumilast-voriconazole-and-zopiclone
#4
Poonam Giri, Sneha Naidu, Nirmal Patel, Harilal Patel, Nuggehally R Srinivas
BACKGROUND AND OBJECTIVES: The role of metabolite(s) to elicit potential clinical drug-drug interaction (DDI) via cytochrome P450 enzymes (CYP) is gaining momentum. In this context, the role of N-oxides for in vitro CYP inhibition has not been evaluated. The objectives of this study were: (a) to examine in vitro CYP inhibition of N-oxides of clozapine, levofloxacin, roflumilast, voriconazole and zopiclone in a tiered approach and (b) evaluate in vitro fate of aforementioned N-oxides examined in recombinant CYPs, human microsomes and hepatocytes...
November 16, 2016: European Journal of Drug Metabolism and Pharmacokinetics
https://www.readbyqxmd.com/read/27848195/acknowledgements
#5
(no author information available yet)
No abstract text is available yet for this article.
November 15, 2016: European Journal of Drug Metabolism and Pharmacokinetics
https://www.readbyqxmd.com/read/27815731/hepatic-uptake-mechanism-of-ophiopogonin-d-mediated-by-organic-anion-transporting-polypeptides
#6
Wen Zhang, Xiaomin Xiong, Lin Chen, Mingyi Liu, Yuqing Xiong, Hong Zhang, Shibo Huang, Chunhua Xia
BACKGROUND AND OBJECTIVES: Ophiopogonin D (OPD) is one of the main active ingredients of SMI (Shenmai injection) which is widely used in clinical practice in China. Our previous study indicated  that OPD might be transported from blood into liver mediated by organic anion transporting polypeptides (OATPs/oatps). This study aims to explore the hepatic uptake mechanism of OPD in rat and human. METHODS: Rosuvastatin (a competitive inhibitor of oatp1b2, oatp1a1, and oatp1a4), glycyrrhizic acid (a specific inhibitor of oatp1b2), digoxin (a specific inhibitor of oatp1a4), bromosulfophthalein (BSP), and ibuprofen (a specific inhibitor of oatp1a1) were used to study the uptake of OPD in rat hepatocytes...
November 4, 2016: European Journal of Drug Metabolism and Pharmacokinetics
https://www.readbyqxmd.com/read/27778300/liver-perfusion-modifies-gd-dtpa-and-gd-bopta-hepatocyte-concentrations-through-transfer-clearances-across-sinusoidal-membranes
#7
Jean-Luc Daire, Benjamin Leporq, Valérie Vilgrain, Bernard E Van Beers, Sabine Schmidt, Catherine M Pastor
BACKGROUND AND OBJECTIVES: Gadobenate dimeglumine (Gd-BOPTA) is a commercialised hepatobiliary contrast agent used during liver magnetic resonance imaging (MRI) to detect liver diseases. It enters into human hepatocytes through organic anion transporting polypeptides (OATP1B1/B3) and crosses the canalicular transporter multiple resistance-associated protein 2 (MRP2) to be excreted into bile canaliculi. Gd-BOPTA can return to sinusoids via the sinusoidal transporters MRP3/MRP4. Hepatocyte concentrations of Gd-BOPTA depend on three clearances: the sinusoidal clearance or volume of sinusoidal blood cleared of drugs per unit of time and two hepatocyte clearances (into bile canaliculi or back to sinusoids) or volume of hepatocytes cleared of drugs per unit of time in the respective liver compartments...
October 24, 2016: European Journal of Drug Metabolism and Pharmacokinetics
https://www.readbyqxmd.com/read/27744636/identification-of-naringin-metabolites-in-human-urine-and-feces
#8
Xuan Zeng, Yang Bai, Wei Peng, Weiwei Su
BACKGROUND AND OBJECTIVES: Naringin, an active flavanone glycoside, has been widely considered as a prospective antitussive and expectorant. The present study aimed to elucidate the metabolic profile of naringin in the human body. METHODS: Four male and three female volunteers (20-30 years old and 18.8-21.7 kg/m(2) Body Mass Index) were orally administrated 320 mg naringin; their urine and feces were collected at different times and the corresponding metabolites were identified with a high resolution ultra-fast liquid chromatography-quadrupole-time-of-flight tandem mass spectrometry (UFLC-Q-TOF-MS/MS) system...
October 15, 2016: European Journal of Drug Metabolism and Pharmacokinetics
https://www.readbyqxmd.com/read/27743266/erratum-to-population-pharmacokinetic-modeling-of-oxcarbazepine-active-metabolite-in-chinese-patients-with-epilepsy
#9
Yunli Yu, Quanying Zhang, Wenjun Xu, Chengzhe Lv, Gang Hao
No abstract text is available yet for this article.
October 14, 2016: European Journal of Drug Metabolism and Pharmacokinetics
https://www.readbyqxmd.com/read/27734327/pharmacokinetics-and-pharmacodynamics-of-promising-arginase-inhibitors
#10
Khaled S Abdelkawy, Kelsey Lack, Fawzy Elbarbry
Up-regulation of arginase activity in several chronic disease conditions, including cancer and hypertension, may suggest new targets for treatment. Recently, the number of new arginase inhibitors with promising therapeutic effects for asthma, cancer, hypertension, diabetes mellitus, and erectile dysfunction has shown a remarkable increase. Arginase inhibitors may be chemical substances, such as boron-based amino acid derivatives, α-difluoromethylornithine (DMFO), and Nω-hydroxy-nor-L-arginine (nor-NOHA) or, of plant origin such as sauchinone, salvianolic acid B (SAB), piceatannol-3-O-β-D-glucopyranoside (PG) and obacunone...
October 12, 2016: European Journal of Drug Metabolism and Pharmacokinetics
https://www.readbyqxmd.com/read/27686853/mixed-micelles-loaded-with-bile-salt-an-approach-to-enhance-intestinal-transport-of-the-bcs-class-iii-drug-cefotaxime-in-rats
#11
Mosab Arafat, Cathrin Kirchhoefer, Momir Mikov
BACKGROUND AND OBJECTIVES: Cefotaxime is a class III drug according to the Biopharmaceutical Classification System due to low intestinal permeability based on poor oral bioavailability. Bile salt compounds have been shown to be effective additive for drug permeation through several biological membranes. The main purpose of this study was to investigate the ability of a mixed micelles made of phosphatidylcholine, sodium deoxycholate, and loaded with a cefotaxime-3α,7α-dihydroxy-12-keto-5β-cholanate complex to enhance the oral bioavailability of cefotaxime in rats...
September 29, 2016: European Journal of Drug Metabolism and Pharmacokinetics
https://www.readbyqxmd.com/read/27683187/enhancement-of-curcumin-bioavailability-via-the-prodrug-approach-challenges-and-prospects
#12
Pahweenvaj Ratnatilaka Na Bhuket, Asma El-Magboub, Ian S Haworth, Pornchai Rojsitthisak
Curcumin is a natural product with many interesting pharmacological properties. However, these are offset by the particularly poor biopharmaceutical properties. The oral bioavailability of curcumin in humans is very low, mainly due to low solubility, poor stability, and extensive metabolism. This has led to multiple approaches to improve bioavailability, including administration of curcumin with metabolism inhibitors, formulation into nanoparticles, modification of the curcumin structure, and development of curcumin prodrugs...
September 28, 2016: European Journal of Drug Metabolism and Pharmacokinetics
https://www.readbyqxmd.com/read/27683186/combined-influence-of-genetic-polymorphism-and-dna-methylation-on-abcb1-expression-and-function-in-healthy-chinese-males
#13
Lan-Xiang Wu, Hong-Bo Zhao, Chun-Jie Wen, Ying Li, Ying-Ying Shao, Zhu Yang, Hong-Hao Zhou
BACKGROUND AND OBJECTIVES: It is well known that the expression and function of ATP-binding cassette transporter B1 (ABCB1) show high interindividual variability, but the reasons have not yet been fully elucidated. In this study, combined influence of genetic polymorphism and DNA methylation on ABCB1 mRNA expression and digoxin pharmacokinetics in healthy Chinese males was analyzed. METHODS: A total of 93 subjects who were homozygous for the ABCB1 1236-2677-3435 TTT or CGC haplotype were enrolled in this study...
September 28, 2016: European Journal of Drug Metabolism and Pharmacokinetics
https://www.readbyqxmd.com/read/27677732/clinical-pharmacokinetics-of-mycophenolic-acid-in-hematopoietic-stem-cell-transplantation-recipients
#14
Daping Zhang, Diana S-L Chow
Mycophenolate mofetil (MMF), an ester prodrug of mycophenolic acid (MPA), is widely used as a maintenance immunosuppressive regimen in solid organ transplant patients. It is increasingly used for the prophylaxis and treatment of graft-versus-host disease (GVHD) in hematopoietic stem cell transplantation (HSCT) patients. MPA displays extensive binding to serum albumin and glucuronidation to the inactive MPA-7-O-glucuronide (MPAG). Here, we review and discuss the pertinent information regarding the clinical pharmacokinetics of MPA in HSCT patients...
September 27, 2016: European Journal of Drug Metabolism and Pharmacokinetics
https://www.readbyqxmd.com/read/27623996/review-of-pharmacokinetic-data-of-different-drug-classes-in-goto-kakizaki-rats-a-non-obese-model-for-type-2-diabetes-mellitus-case-studies-and-perspectives
#15
Harilal Patel, Poonam Giri, Nuggehally R Srinivas
Goto-Kakizaki (GK) rats represent a unique non-obese and lean model with manifestation of type 2 diabetes (T2DM) broadly mimicking the human T2DM development. Therefore, in addition to the use of GK rats to test the efficacy of drugs, it may represent a great tool to study the influence of altered physiological process and/or organ specific pathophysiological changes (i.e., liver, kidney, etc.) on the disposition of drugs. The objectives of the review were: (a) to compile the published pharmacokinetic data of several drugs, such as cephalexin, cyclosporine, exendin-4, gliclazide, grepafloxacin, rosuvastatin, salsalate, salicylic acid, and theophylline, in GK rats relative to normal rats; and (b) critically evaluate the possible role of physiologically altered processes on the pharmacokinetics of reviewed drugs...
September 13, 2016: European Journal of Drug Metabolism and Pharmacokinetics
https://www.readbyqxmd.com/read/27604118/increased-intestinal-absorption-of-genistein-by-coadministering-verapamil-in-rats
#16
Baogang Xie, Huiyun Wang, Huiqin Zou, Yalan Liu, Xiangyu Kong, Xiuzhong Fang
Combination of genistein (GT) and verapamil, a P-glycoprotein (P-gp) inhibitor, can increase GT absorption in situ perfusion technology in rat. To date, little information is yet available about the effect of verapamil on oral absorption of GT in vivo. In this study, a simple and reproducible HPLC-UV method was developed and validated for determination of total GT in rat plasma. Based on this, a pharmacokinetic experiment was designed to characterize biopharmaceutical properties of GT with or without coadministration of verapamil (10...
October 2016: European Journal of Drug Metabolism and Pharmacokinetics
https://www.readbyqxmd.com/read/27086359/clinical-drug-drug-pharmacokinetic-interaction-potential-of-sucralfate-with-other-drugs-review-and-perspectives
#17
Suresh P Sulochana, Muzeeb Syed, Devaraj V Chandrasekar, Ramesh Mullangi, Nuggehally R Srinivas
Sucralfate, a complex of aluminium hydroxide with sulfated sucrose, forms a strong gastrointestinal tract (GIT) mucosal barrier with excellent anti-ulcer property. Because sucralfate does not undergo any significant oral absorption, sucralfate resides in the GIT for a considerable length of time. The unabsorbed sucralfate may alter the pharmacokinetics of the oral drugs by impeding its absorption and reducing the oral bioavailability. Because of the increased use of sucralfate, it was important to provide a reappraisal of the published clinical drug-drug interaction studies of sucralfate with scores of drugs...
October 2016: European Journal of Drug Metabolism and Pharmacokinetics
https://www.readbyqxmd.com/read/26294172/pharmacokinetics-and-tolerability-of-rufinamide-following-single-and-multiple-oral-doses-and-effect-of-food-on-pharmacokinetics-in-healthy-chinese-subjects
#18
Mingzhen Xu, Yang Ni, Ying Zhou, Xiaomeng He, Huqun Li, Hui Chen, Weiyong Li
BACKGROUND: Rufinamide is a triazole derivative that is structurally unrelated to currently marketed antiepileptic medications for add-on treatment of seizures in the setting of Lennox-Gastaut syndrome in patients from the age of 4 years. OBJECTIVE: The purpose of this study was to determine the pharmacokinetic and safety profile of single and multiple doses of rufinamide in healthy Chinese subjects. The effects of food and gender on the pharmacokinetic properties of rufinamide were also evaluated...
October 2016: European Journal of Drug Metabolism and Pharmacokinetics
https://www.readbyqxmd.com/read/26253156/microbial-metabolism-of-atovaquone-and-cytotoxicity-of-the-produced-phase-i-metabolite
#19
Eliane de Oliveira Silva, Natália Dos Santos Gonçalves, Raquel Alves Dos Santos, Niege Araçari Jacometti Cardoso Furtado
BACKGROUND AND OBJECTIVES: Atovaquone is a hydroxynaphthoquinone with selective action in the mitochondrial respiratory chain of malaria parasite. It is employed for both the treatment and prevention of malaria, in a combination with proguanil. The aim of this study was to elucidate the in vitro metabolites from atovaquone and to evaluate their cytotoxic activities. METHODS: The biotransformation of atovaquone was performed using Mucor rouxii NRRL 1894, Cunninghamella echinulata var...
October 2016: European Journal of Drug Metabolism and Pharmacokinetics
https://www.readbyqxmd.com/read/26189007/population-pharmacokinetic-analysis-of-the-oral-absorption-process-and-explaining-intra-subject-variability-in-plasma-exposures-of-imatinib-in-healthy-volunteers
#20
Ali-Akbar Golabchifar, Saeed Rezaee, Nahid Mobarghei Dinan, Abbas Kebriaeezadeh, Mohammad-Reza Rouini
BACKGROUND AND OBJECTIVE: Imatinib mesylate is presently the first-line treatment for chronic myeloid leukemia (CML). The aim of this study was to investigate the absorption and distribution kinetics of imatinib in healthy Iranian volunteers using nonlinear mixed effects modeling (NLMEM) to assess the overall, intra- and inter-subject variabilities in pharmacokinetic parameters after oral administration. METHODS: This analysis was based on data from 24 healthy subjects who participated in a bioequivalence study after administering a single dose of 200 mg of each formulation...
October 2016: European Journal of Drug Metabolism and Pharmacokinetics
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